Several salts of olanzapine, including olanzapine malonate, olanzapine glycolate, olanzapine maleate, and olanzapine benzoate, have been found to have favorable solid state characteristics.

This invention encompasses methods of synthesizing olanzapine without solvents or by using low boiling organic solvents.

The present invention provides a process for preparing olanzapine and intermediates therefor.

Methods and compositions are disclosed utilizing olanzapine-N-oxide for the treatment of psychosis in humans. Olanzapine-N-oxide exhibits a lessened liability toward drug-drug interactions than olanzapine and a more predictable dosing regimen than olanzapine. Olanzapine-N-oxide is also useful for the treatment of acute mania, mild anxiety states, anxiety disorders, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder, autistic disorder, excessive aggression, substance abuse,...

A process for the preparation of polymorph Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine, or olanzapine.

The present invention provides a method for treating migraine pain comprising administering an analgesic dosage of olanzapine.

Methods and compositions are disclosed utilizing olanzapine-N-oxide for the treatment of psychosis in humans. Olanzapine-N-oxide exhibits a lessened liability toward drug-drug interactions than olanzapine and a more predictable dosing regimen than olanzapine. Olanzapine-N-oxide is also useful for the treatment of acute mania, mild anxiety states, anxiety disorders, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder, autistic disorder, excessive aggression, substance abuse,...

The invention relates to the discovery that pamoate salts of haloperidol and aripiprazole result in a good to superior long acting and/or extended release profile. Thus, in one aspect of the invention, the invention includes pamoate salts of haloperidol or aripiprazole. Preferably, the pamoate salt is characterized by a ratio of haloperidol to pamoate of 1:1 or 2:1. The pamoate salt can be crystalline, such as a needle or a dense crystal, such as described in the Figures.The invention further re...

The invention is directed to a series of novel crystalline olanzapine forms, in particular hydrated and solvated crystalline forms of olanzapine, methods of use in pharmaceutical compositions, and method of treating psychiatric disorders using the crystalline forms. One series of the crystalline forms are hydrates, i.e. water containing crystals, wherein water may be present in a ratio of about 2:1.5 to a ratio of about 1:3 olanzapine:water, while another includes solvates such as an isobutanol ...

The invention relates to the methods for preparation of olanzapine polymorphic Form I. The invention also provides new mixed solvates of olanzapine, which are valuable intermediates used in the preparation of pure olanzapine polymorphic Form I.